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Silanetriols as in vitro inhibitors for AChE.

ABSTRACT: Three stable silanetriols with increasing steric protection of the silicon atom have been tested for inhibition of acetylcholinesterase (AChE). For all tested silanetriols we found reversible inhibition of the AChE activity at a 100 ?M concentration. The highest inhibition rate was found for the sterically least hindered cyclohexylsilanetriol with 45% inhibition relative to galanthamine hydrobromide for which an IC(50) value of 121 ± 3 ?M was determined as well. The cytotoxicity of the silanetriols used was found to be negligible at concentrations relevant for inhibition.

SUBMITTER: Blunder M

PROVIDER: S-EPMC3013380 | biostudies-literature | 2011 Jan

REPOSITORIES: biostudies-literature

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Silanetriols as in vitro inhibitors for AChE.

Blunder Martina M Hurkes Natascha N Spirk Stefan S List Martina M Pietschnig Rudolf R

Bioorganic & medicinal chemistry letters 20101105 1

Three stable silanetriols with increasing steric protection of the silicon atom have been tested for inhibition of acetylcholinesterase (AChE). For all tested silanetriols we found reversible inhibition of the AChE activity at a 100 μM concentration. The highest inhibition rate was found for the sterically least hindered cyclohexylsilanetriol with 45% inhibition relative to galanthamine hydrobromide for which an IC(50) value of 121 ± 3 μM was determined as well. The cytotoxicity of the silanetri ...[more]

PMID: 21111617

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